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PDK4-IN-1 hydrochloride  ≥98%

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包装规格：5mg 10mg 25mg 50mg 100mg in glass bottle
溶解性：溶于DMSO（125 mg/mL 超声）
产品描述：基本信息 产品编号：P10821 产品名称：PDK4-IN-1 hydrochloride CAS: 2310262-11-2   储存条件 粉末 -20℃ 四年     分子式： C22H20ClN3O2 溶于液体 -80℃ 六个月 分子量 393.87 -20℃ 一个月 化学名：      Solubility (25°C)   体外 DMSO   Ethanol   Water   体内（现配现用）     ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 2.5389mL 12.6945mL 25.3891mL 5mM 0.5078mL 2.5389mL 5.0778mL 10mM 0.2539mL 1.2695mL 2.5389mL   生物活性 产品描述 一种蒽醌衍生物，也是一种有效的，口服活性的丙酮酸脱氢酶激酶 4 (PDK4) 抑制剂，IC50 值为 84nM。 靶点/IC50 IC50: 84nM (Pyruvate dehydrogenase kinase 4(PDK4)) 体外研究 PDK4-IN-1 (Compound 8c; 50μM; 0-72 hours; HCT116 and RKO cells) treatment significantly impedes the proliferation of human colon cancer cell lines, HCT116 and RKO. The colony formation efficiency in HCT116 and RKO cells Is significantly reduced after treatment of PDK4-IN-1.PDK4-IN-1 (Compound 8c; 10-50μM; 24 hours; HCT116 and RKO cells) treatment dose-dependently increased apoptosis.PDK4-IN-1 (Compound 8c; 10μM; 24 hours; HEK293T cells) treatment inhibits phosphorylation of Ser232, Ser293, and Ser300 of PDHE1α.10μM of PDK4-IN-1 (Compound 8c) significantly increases p-Akt in AML12 cells.PDK4-IN-1 (compound 8c)-induced phosphorylation of p53 on serine 15 is a dose-dependent response in both HCT116 and RKO cells.PDK4-IN-1 decreases the expression of BCL-xL and increases the expression of BAX. Cleavage of PARP1 and caspase 3 are increased by PDK4-IN-1.Cell Viability Assay Cell Line: HCT116 and RKO cells Concentration: 50μM Incubation Time: 0 hour, 24 hours,48 hours,72hours Result: Significantly impeded the proliferation of human colon cancer cell lines, HCT116 and RKO. Apoptosis Analysis Cell Line: HCT116 and RKO cells Concentration: 10μM, 25μM, 50μM Incubation Time: 24 hours Result: Dose-dependently increased apoptosis. Western Blot Analysis Cell Line: HEK293T human embryonic kidney cells Concentration: 10μM Incubation Time: 24 hours Result: Inhibited phosphorylation of Ser232, Ser293, and Ser300 of PDHE1α 体内研究 PDK4-IN-1 (Compound 8c; 100mg/kg; oral administration; daily; for 1 week; C57BL/6J mice) treatment significantly improves glucose tolerance.Pre-incubation with PDK4-IN-1 (compound 8c) dose-dependently inhibits the release of β-hexosaminidase from IgE/antigenactivated BMMCs,showing that the absorbance values are 0.26, 0.20, and 0.126 in IgE/Ag, 10μM, and 20μM PDK4-IN-1-treated BMMCs.The pharmacokinetic (PK) profiles of PDK4-IN-1 (compound 8c) are evaluated in rat. PDK4-IN-1 shows good bioavailability (64%), long half-life (>7h), and moderate clearance (CL of 0.69) in rats. Animal Model: C57BL/6J mice (8-week old) fed with high-fat diet Dosage: 100mg/kg Administration: Oral administration;daily;for 1 week Result: Significantly improved glucose tolerance.
保存条件：-20℃

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